EC0489 

EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor^[1]. Small molecule-agent conjugate (SMDC)^[2].

Folate receptor^[1]

The affinity of EC0489 toward the folate receptor (FR) is approximately half of that of folic acid (relative affinity 0.50)^[1].

FR-positive KB cells are highly sensitive to EC0489 with an IC₅₀ of 5 nM^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

EC0489 has a favorable toxicology profile in Rats. EC0489 (2, 3, and 4 μmol/kg) has antitumor activity against mice KB tumor models in a dose-dependent manner^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

2550.68

C₁₁₁H₁₅₆N₂₂O₄₃S₂

1096702-14-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Leamon CP, et al. Reducing undesirable hepatic clearance of a tumor-targeted vinca alkaloid via novel saccharopeptidic modifications. J Pharmacol Exp Ther. 2011 Feb;336(2):336-43.  [Content Brief]

  [2]. Zhuang C, et al. Small molecule-drug conjugates: A novel strategy for cancer-targeted treatment. Eur J Med Chem. 2019 Feb 1;163:883-895.  [Content Brief]